Neostigmine
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Image:Neostigmine.png | |
| (m-hydroxyphenyl)trimethyl-, dimethylcarbamate(ester) ammonium | |
| CAS number 59-99-4 | ATC code N07AA01, S01EB06 |
| Chemical formula | C12H19N2O2 |
| Molecular weight | 223.294 |
| Bioavailability | Unclear, probably less than 5% |
| Metabolism | Slow hydrolysis by acetylcholinesterase and also by plasma esterases |
| Elimination half-life | 50-90 minutes |
| Excretion | Unchanged drug (up to 70%) and alcoholic metabolite (30%) are excreted in the urine |
| Pregnancy category | ? |
| Legal status | ? |
| Routes of administration | ? |
Neostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors.
Clinical Uses
It is used to improve muscle tone in people with myasthenia gravis and routinely in anesthesia at the end of an operation to reverse the effects of non-depolarising muscle relaxants such as vecuronium.
It can also be used for urinary retention resulting from general anaesthetia and to treat curariform drug toxicity.
Another indication for use is the Ogilvie syndrome which is a pseudoobstruction of the colon in critically ill patients.
Neostigmine will cause slowing of the heart rate (bradycardia), for this reason it is usually given along with a parasympatholytic drug such as atropine or glycopyrrolate.
Neostigmine is available under several trade names such as Prostigmin®.
Sources
- Brenner, G. M. (2000). Pharmacology. Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6
- Canadian Pharmacists Association (2000). Compendium of Pharmaceuticals and Specialties (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4